ZM241385 is a novel non-xanthine adenosine receptor antagonist with selectivity for the A2a receptor subtype. ZM-241385 significantly blunts the hypotensive effects of CCPA and NECA without altering the bradycardia induced by these agonists. It blocks the infarct size-reducing effects(cardioprotective effects) of this two distinct adenosine receptor agonists.
In vitro: ZM-241385 exhibits high potency for A2a receptor-mediated effects versus A1 receptor-mediated effects. A2AR agonist CGS21680 dramatically up-regulated A2AR mRNA; this response was reversed by concurrent exposure to ZM241385.
Redox Rep. 2022 Dec;27(1):270-278.
Caffeine reduces oxidative stress to protect against hyperoxia-induced lung injury via the adenosine A2A receptor/cAMP/PKA/Src/ERK1/2/p38MAPK pathway
ZM241385 purchased from AbMole
Molecules. 2022 May 6;27(9):2994.
Inosine and D-Mannose Secreted by Drug-Resistant Klebsiella pneumoniae Affect Viability of Lung Epithelial Cells
ZM241385 purchased from AbMole
| Molecular Weight | 337.34 |
| Formula | C16H15N7O2 |
| CAS Number | 139180-30-6 |
| Solubility (25°C) | DMSO 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Adenosine Receptor Products |
|---|
| LUF5519
LUF5519 is a ribose-containing adenosine A1 receptor agonist. |
| LUF6258
LUF6258 is a hybrid ortho/allosteric ligand of the adenosine A(1) receptor. |
| A3AR agonist 1
A3AR agonist 1 is an A3AR agonist (Ki: 25.8 nM). |
| A3AR agonist 2
A3AR agonist 2 a selective A3AR agonist (Ki: 22.1 nM). |
| Inupadenant hydrochloride
Inupadenant (EOS-850) hydrochloride is an orally active, highly selective A2A receptor antagonist. |
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